Title:Bromodomain-Containing Protein 4: A Druggable Target
VOLUME: 20 ISSUE: 15
Author(s):Yingying Shi, Jingwen Liu, Yuanyuan Zhao, Jiaoxian Cao, Yiming Li* and Fujiang Guo*
Affiliation:School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201203
Keywords:Bromodomain-containing protein 4, small molecule inhibitors, pharmacology, tumor, coronary heart disease, natural
products, synthetic compounds.
Abstract:Bromodomain-containing protein 4 (BRD4) belongs to the bromodomain and extraterminal
family. BRD4 inhibitors can regulate acetylated lysine and form protein complexes that initiate
transcriptional programs as an epigenetic regulator of the histone code. BRD4 was initially considered
to be one of the most promising targets for combating malignant tumors. However, many recent
studies have shown that BRD4 plays a crucial role in various kinds of diseases, including cancer, coronary
heart disease, neurological disorder, and obesity. Currently, several BRD4 inhibitors are undergoing
clinical trials. A search for new BRD4 inhibitors appears to be of great utility for developing
novel drugs. In this mini-review, we highlight the inhibitors of BRD4 from natural products and synthesized
sources, as well as their applications in cancer, glucolipid metabolism, inflammation, neuronal
stimulation activation, human immunodeficiency virus and renal fibrosis.